Parsaclisib free base | INCB050465 | CAS#1426698-88-5 | PI3Kδ inhibitor

MedKoo Cat#: 206505 | Name: Parsaclisib free base

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Parsaclisib, also known as INCB050465, is a novel PI3Kδ inhibitor which synergizes with PIM protein kinase inhibition to cause tumor regression in a model of DLBCL. INCB050465 inhibits PI3Kδ (IC50 = 1 nM at 1 mM ATP) with approximately 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases. INCB050465 demonstrates potent activity with IC50 values ranging from 0.2 to 2 nM. In addition, INCB050465 blocks the proliferation of several DLBCL and MCL cell lines in vitro (EC50 < 10 nM) and can slow tumor growth in the Pfeiffer model of DLBCL in vivo.

Chemical Structure

Parsaclisib free base

CAS#1426698-88-5 (free base)

Theoretical Analysis

MedKoo Cat#: 206505

Name: Parsaclisib free base

CAS#: 1426698-88-5 (free base)

Chemical Formula: C20H22ClFN6O2

Exact Mass: 432.1477

Molecular Weight: 432.88

Elemental Analysis: C, 55.49; H, 5.12; Cl, 8.19; F, 4.39; N, 19.41; O, 7.39

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 580.00	2 Weeks
10mg	USD 960.00	2 Weeks

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Related CAS #

1426698-88-5 (free base) 1995889-48-9 (HCl)

Synonym

INCB50465 HCl; INCB-50465; INCB 50465; IINCB050465; INCB-050465; INCB 050465. INCB050465 free base; Parsaclisib; Parsaclisib free base

IUPAC/Chemical Name

(4R)-4-{3-[(1S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-fluorophenyl}pyrrolidin-2-one

InChi Key

ZQPDJCIXJHUERQ-QWRGUYRKSA-N

InChi Code

InChI=1S/C20H22ClFN6O2/c1-4-30-18-12(6-13(21)17(22)16(18)11-5-14(29)24-7-11)10(3)28-20-15(9(2)27-28)19(23)25-8-26-20/h6,8,10-11H,4-5,7H2,1-3H3,(H,24,29)(H2,23,25,26)/t10-,11-/m0/s1

SMILES Code

O=C1NC[C@@H](C2=C(F)C(Cl)=CC([C@@H](N3N=C(C)C4=C(N)N=CN=C43)C)=C2OCC)C1

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 432.88 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Sancho JM, Abrisqueta P, Kumar A, Cordoba R, Tani M, Langmuir P, Rappold E, Liu T, Lopez-Guillermo A. Safety and efficacy of parsaclisib in combination with rituximab, bendamustine + rituximab, or ibrutinib in patients with previously treated B-cell lymphoma: analysis of a phase 1 dose-finding study (CITADEL‑112). Leuk Lymphoma. 2024 Jul;65(7):911-921. doi: 10.1080/10428194.2024.2331626. Epub 2024 Apr 10. PMID: 38598516. 2: Li V, Yap GPA, Ni C. Crystal structure of (S)-5-(3-acetyl-5-chloro-2-ethoxy-6-fluorophenyl)-2-oxazolidinone. Acta Crystallogr E Crystallogr Commun. 2024 Mar 19;80(Pt 4):375-377. doi: 10.1107/S2056989024001920. PMID: 38584728; PMCID: PMC10993593. 3: Munster P, Iannotti N, Cho DC, Kirkwood JM, Villaruz LC, Gibney GT, Hodi FS, Mettu NB, Jones M, Bowman J, Smith M, Lakshminarayanan M, O'Day S. Correction: Combination of Itacitinib or Parsaclisib with Pembrolizumab in Patients with Advanced Solid Tumors: A Phase I Study. Cancer Res Commun. 2024 Mar 13;4(3):785. doi: 10.1158/2767-9764.CRC-24-0133. Erratum for: Cancer Res Commun. 2023 Dec 19;3(12):2572-2584. doi: 10.1158/2767-9764.CRC-22-0461. PMID: 38477691; PMCID: PMC10936421. 4: Li J, Gong X, Liu X, Liu X, Szeto K, Chen X. Evaluation of the cardiac safety of parsaclisib, a selective PI3Kδ inhibitor, in patients with previously treated B-cell malignancies: Results from the CITADEL-101 study. Pharmacol Res Perspect. 2024 Apr;12(2):e1165. doi: 10.1002/prp2.1165. PMID: 38407508; PMCID: PMC10895684. 5: Yacoub A, Borate U, Rampal RK, Ali H, Wang ES, Gerds AT, Hobbs G, Kremyanskaya M, Winton E, O'Connell C, Goel S, Oh ST, Schiller G, McCloskey J, Palmer J, Holmes H, Hager S, Assad A, Erickson-Viitanen S, Zhou F, Daver N. Phase 2 study of add-on parsaclisib for patients with myelofibrosis and suboptimal response to ruxolitinib: final results. Blood Adv. 2024 Mar 26;8(6):1515-1528. doi: 10.1182/bloodadvances.2023011620. PMID: 38290135; PMCID: PMC10966172. 6: Munster P, Iannotti N, Cho DC, Kirkwood JM, Villaruz LC, Gibney GT, Hodi FS, Mettu NB, Jones M, Bowman J, Smith M, Lakshminarayanan M, O'Day S. Combination of Itacitinib or Parsaclisib with Pembrolizumab in Patients with Advanced Solid Tumors: A Phase I Study. Cancer Res Commun. 2023 Dec 19;3(12):2572-2584. doi: 10.1158/2767-9764.CRC-22-0461. Erratum in: Cancer Res Commun. 2024 Mar 13;4(3):785. doi: 10.1158/2767-9764.CRC-24-0133. PMID: 38115208; PMCID: PMC10729644. 7: Phillips TJ, Avigdor A, Gurion R, Patti C, Corradini P, Tani M, Mehta A, Lossos IS, Zinzani PL, Thieblemont C, Jurczak W, Zheng F, Rappold E, Zhao W, Jiang P, Johnson P. A phase 2 study of the PI3Kδ inhibitor parsaclisib in relapsed and refractory marginal zone lymphoma (CITADEL-204). Blood Adv. 2024 Feb 27;8(4):867-877. doi: 10.1182/bloodadvances.2023010648. PMID: 38113459; PMCID: PMC10875254. 8: Witkowska M, Majchrzak A, Robak P, Wolska-Washer A, Robak T. Metabolic and toxicological considerations for phosphoinositide 3-kinase delta inhibitors in the treatment of chronic lymphocytic leukemia. Expert Opin Drug Metab Toxicol. 2023 Sep;19(9):617-633. doi: 10.1080/17425255.2023.2260305. Epub 2023 Sep 15. PMID: 37714711. 9: Trněný M, Avigdor A, McKinney MS, Paneesha S, Wahlin BE, Hrom JS, Cunningham D, Morley N, Canales M, Bastos-Oreiro M, Belada D, Devizzi L, Zheng F, DeMarini DJ, Jiang W, Jiang P, Lynch RC. Parsaclisib, a PI3Kδ inhibitor, in relapsed and refractory follicular lymphoma (CITADEL-203): a phase 2 study. EClinicalMedicine. 2023 Aug 18;63:102130. doi: 10.1016/j.eclinm.2023.102130. PMID: 37662520; PMCID: PMC10469382. 10: Zinzani PL, Trněný M, Ribrag V, Zilioli VR, Walewski J, Christensen JH, Delwail V, Rodriguez G, Venugopal P, Coleman M, Dartigeas C, Patti C, Pane F, Jurczak W, Taszner M, Paneesha S, Zheng F, DeMarini DJ, Jiang W, Gilmartin A, Mehta A. Parsaclisib, a PI3Kδ inhibitor, in relapsed and refractory mantle cell lymphoma (CITADEL-205): a phase 2 study. EClinicalMedicine. 2023 Aug 10;62:102131. doi: 10.1016/j.eclinm.2023.102131. PMID: 37599908; PMCID: PMC10433033. 11: Hamadani M, Coleman M, Boccia R, Duras J, Hutchings M, Zinzani PL, Cordoba R, Oreiro MB, Williams V, Liu H, Stouffs M, Langmuir P, Sancho JM. Safety and efficacy of parsaclisib in combination with obinutuzumab and bendamustine in patients with relapsed or refractory follicular lymphoma (CITADEL-102): A phase 1 study. Hematol Oncol. 2023 Dec;41(5):848-857. doi: 10.1002/hon.3209. Epub 2023 Jul 26. PMID: 37496298. 12: Chifotides HT, Masarova L, Verstovsek S. SOHO State of the Art Updates and Next Questions: Novel Therapeutic Strategies in Development for Myelofibrosis. Clin Lymphoma Myeloma Leuk. 2023 Apr;23(4):219-231. doi: 10.1016/j.clml.2022.12.014. Epub 2023 Jan 6. PMID: 36797153; PMCID: PMC10378306. 13: Fattizzo B, Motta I. Rise of the planet of rare anemias: An update on emerging treatment strategies. Front Med (Lausanne). 2023 Jan 9;9:1097426. doi: 10.3389/fmed.2022.1097426. PMID: 36698833; PMCID: PMC9868867. 14: Correction: Exploring the safety, effect on the tumor microenvironment, and efficacy of itacitinib in combination with epacadostat or parsaclisib in advanced solid tumors: a phase I study. J Immunother Cancer. 2022 Oct;10(10):e004223corr1. doi: 10.1136/jitc-2021-004223corr1. Erratum for: J Immunother Cancer. 2022 Mar;10(3):e004223. doi: 10.1136/jitc-2021-004223. PMID: 36283739; PMCID: PMC9608536. 15: Ghorbanalipoor S, Emtenani S, Parker M, Kamaguchi M, Osterloh C, Pigors M, Gross N, Khil'chenko S, Kasprick A, Patzelt S, Wortmann D, Ibrahim IO, Izumi K, Goletz S, Boch K, Kalies K, Bieber K, Smith P, Schmidt E, Ludwig RJ. Cutaneous kinase activity correlates with treatment outcomes following PI3K delta inhibition in mice with experimental pemphigoid diseases. Front Immunol. 2022 Sep 28;13:865241. doi: 10.3389/fimmu.2022.865241. Erratum in: Front Immunol. 2022 Nov 30;13:1099535. doi: 10.3389/fimmu.2022.1099535. PMID: 36248903; PMCID: PMC9555174. 16: Fattizzo B, Barcellini W. New Therapies for the Treatment of Warm Autoimmune Hemolytic Anemia. Transfus Med Rev. 2022 Oct;36(4):175-180. doi: 10.1016/j.tmrv.2022.08.001. Epub 2022 Sep 6. PMID: 36182620. 17: Skånland SS, Brown JR. PI3K inhibitors in chronic lymphocytic leukemia: where do we go from here? Haematologica. 2023 Jan 1;108(1):9-21. doi: 10.3324/haematol.2022.281266. PMID: 35899388; PMCID: PMC9827175. 18: Gerds AT, Bartalucci N, Assad A, Yacoub A. Targeting the PI3K pathway in myeloproliferative neoplasms. Expert Rev Anticancer Ther. 2022 Aug;22(8):835-843. doi: 10.1080/14737140.2022.2093192. Epub 2022 Jun 29. PMID: 35763287. 19: Kuykendall AT, Komrokji RS. JAK Be Nimble: Reviewing the Development of JAK Inhibitors and JAK Inhibitor Combinations for Special Populations of Patients with Myelofibrosis. J Immunother Precis Oncol. 2021 Jun 22;4(3):129-141. doi: 10.36401/JIPO-20-36. PMID: 35663107; PMCID: PMC9138443. 20: Altman RA, Brai A, Golden J, La Regina G, Li Z, Moore TW, Pomerantz WCK, Rajapaksa NS, Adams AM. An Innovation 10 Years in the Making: The Stories in the Pages of ACS Medicinal Chemistry Letters. ACS Med Chem Lett. 2022 Feb 3;13(4):540-545. doi: 10.1021/acsmedchemlett.1c00623. PMID: 35450346; PMCID: PMC9014514.

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Description:

Chemical Structure

Theoretical Analysis

Price and Availability

Preparing Stock Solutions

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